Page last updated: 2024-11-12

msh, 4-nle-7-phe-alpha-

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID16154396
SCHEMBL ID22463810
MeSH IDM0089944

Synonyms (29)

Synonym
msh, 4-nle-7-phe-alpha-
(nle4,d-phe7)-alpha-msh
4-nle-7-phe-alpha-msh
melanotan-1
alpha-msh, nle(4)-phe(7)-
alpha-melanotropin, 4-l-norleucine-7-d-phenylalanine-
cuv-1647
n-acetyl-l-seryl-l-tyrosyl-l-seryl-l-norleucyl-l-alpha-glutamyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophylglycyl-l-lysyl-l-prolyl-l-valinamide
n-acteyl-l-ser-l-tyr-l-ser-l-nle-l-glu-l-his-d-phe-l-arg-l-trp-gly-l-lys-l-pro-l-val-nh2
melanotan i
cuv1647
ndp-alpha-msh
cuv 1647
ac-ser-tyr-ser-nle-glu-his-d-phe-arg-trp-gly-lys-pro-val-nh2
afamelanotide [usan:inn]
qw68w3j66u ,
afamelanotide [inn]
afamelanotide [orange book]
afamelanotide [who-dd]
.alpha.-melanotropin (swine), 4-l-norleucine-7-d-phenylalanine-
[nle4,d-phe7]-alpha-msh
afamelanotide [mi]
afamelanotide [usan]
melanotan-i
[nle4,d-phe7]--msh
afamelanotidemt-i
[nle4,d-phe7]-a-msh
SCHEMBL22463810
EN300-18527915

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
"A comparative pharmacokinetic trial was performed with a superpotent synthetic melanotropic peptide, [Nle4-D-Phe7]-alpha-MSHi-13 (melanotan-I or MT-I) given by three routes of administration."( Skin pigmentation and pharmacokinetics of melanotan-I in humans.
Aickin, M; Blanchard, J; Brooks, C; Dorr, RT; Hadley, ME; Hruby, VJ; Levine, N; Ugwu, SO, 1997
)
0.3

Compound-Compound Interactions

ExcerptReferenceRelevance
"Three phase 1 clinical trials of a superpotent melanotropic peptide, melanotan-1 (MT-1, or [Nle(4)-D-Phe(7)]alpha-melanocyte-stimulating hormone) were performed to demonstrate safety for MT-1 therapy combined with UV-B light or sunlight."( Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers.
Alberts, DS; Bangert, JL; Brooks, C; Dorr, RT; Ertl, G; Humphrey, S; Levine, N; Powell, MB, 2004
)
0.32
"Open-label studies at 2 dose levels of MT-1 combined with small doses of UV-B to the neck or buttock or full sunlight to half of the back."( Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers.
Alberts, DS; Bangert, JL; Brooks, C; Dorr, RT; Ertl, G; Humphrey, S; Levine, N; Powell, MB, 2004
)
0.32
"Melanotan-1 can be safely combined with UV-B light or sunlight and appears to act synergistically in the tanning response to light."( Effects of a superpotent melanotropic peptide in combination with solar UV radiation on tanning of the skin in human volunteers.
Alberts, DS; Bangert, JL; Brooks, C; Dorr, RT; Ertl, G; Humphrey, S; Levine, N; Powell, MB, 2004
)
0.32

Bioavailability

ExcerptReferenceRelevance
" Finally, transformation of indol-1-yl to indol-3-yl resulted in discovery of a novel highly potent and orally bioavailable ADA inhibitor, 1-[(R)-4-(5-(3-(4-chlorophenyl)propoxy)-1-methylindol-3-yl)-1-hydroxy-2-butyl]imidazole-4-carboxamide 8c."( Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
Kinoshita, T; Kuno, M; Nakanishi, I; Seki, N; Tanaka, K; Terasaka, T, 2004
)
0.32
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves to alpha-MSH were compared in the presence of different calcium concentrations, and Schild regression plots were constructed."( The role of calcium in MSH stimulated melanosome dispersion.
Lucas, AM; Shuster, S; Thody, AJ,
)
0.13
" The dose-response curves for the MSH peptides are sigmoidal and the two peptides are equipotent in their effects on human melanocytes."( Cultured human melanocytes respond to MSH peptides and ACTH.
Donatien, PD; Hunt, G; Kyne, S; Lunec, J; Thody, AJ; Todd, C, 1994
)
0.29
" Pretreatment with ACTH-(1-24) caused a pronounced, dose-dependent parallel shift to the right of the dose-response curve for the pressor and tachycardiac effects of gamma 2-MSH."( Different cardiovascular profiles of three melanocortins in conscious rats; evidence for antagonism between gamma 2-MSH and ACTH-(1-24).
De Wildt, DJ; Kleijne, JA; Van Bergen, P; Versteeg, DH, 1997
)
0.3
" This regimen induced tanning at 3 of 8 anatomic sites including the face, neck and forearm by comparison of baseline to (1) the end of the daily dosing period, (day 14), and (2) one week later, (day 21)."( Increased eumelanin expression and tanning is induced by a superpotent melanotropin [Nle4-D-Phe7]-alpha-MSH in humans.
Alberts, DS; Brooks, C; Dorr, RT; Dvorakova, K; Hruby, V; Levine, N; Lines, R; Miketova, P; Schram, K, 2000
)
0.31
" Dose-response curves of cAMP accumulation were right-shifted for both forms."( Thr40 and Met122 are new partial loss-of-function natural mutations of the human melanocortin 1 receptor.
García-Borrón, JC; Germer, S; González, P; Jiménez-Cervantes, C; Sánchez, CO; Sánchez, J, 2001
)
0.31
" Repetitive once daily oral dosing (0."( Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
Faier, A; Gabinet, Y; Gilon, C; Halbfinger, E; Haskell-Luevano, C; Hess, S; Hoffman, A; Lapidot, T; Linde, Y; Ovadia, O; Portillo, FP; Safrai, E; Shalev, DE; Swed, A; Winkler, I; Xiang, Z; Yarden, D, 2008
)
0.35
" There are questions regarding the preparation, administration, and dosage of these substances."( Risks of unregulated use of alpha-melanocyte-stimulating hormone analogues: a review.
Bergman, W; Habbema, L; Halk, AB; Neumann, M, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
dermatologic drugA drug used to treat or prevent skin disorders or for the routine care of skin.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
polypeptideA peptide containing ten or more amino acid residues.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (12)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Adenosine deaminaseHomo sapiens (human)Ki0.01600.00000.30887.0000AID33850
Melanocortin receptor 4Homo sapiens (human)IC50 (µMol)0.00320.00020.64136.1900AID109111; AID109119; AID109127; AID109128; AID109131; AID1151528; AID1151529; AID1285634; AID1336329; AID1559799; AID242174; AID346427; AID751880; AID752240
Melanocortin receptor 4Homo sapiens (human)Ki0.00250.00000.30864.8860AID109137; AID259534; AID259535; AID259536; AID259537; AID259538; AID259539; AID259540; AID259541; AID259542; AID259543; AID346427; AID632881; AID677161; AID751880
Melanocortin receptor 5Homo sapiens (human)IC50 (µMol)0.00140.00091.25669.5180AID109306; AID109425; AID109428; AID109429; AID240566
Melanocortin receptor 5Homo sapiens (human)Ki0.00520.00053.52658.9290AID632882; AID677160
Melanocortin receptor 3Mus musculus (house mouse)IC50 (µMol)0.00590.00420.00590.0082AID1296529; AID1483091; AID1559790
Melanocortin receptor 5Mus musculus (house mouse)IC50 (µMol)0.14000.14000.14000.1400AID1559796
Melanocortin receptor 3Homo sapiens (human)IC50 (µMol)0.00260.00120.01660.0832AID108787; AID108790; AID108792; AID108794; AID108795; AID242173
Melanocortin receptor 3Homo sapiens (human)Ki0.00070.00010.24522.8650AID108798; AID677159
Melanocortin receptor 4Mus musculus (house mouse)IC50 (µMol)0.00220.00110.05730.2140AID109283; AID1296527; AID1483073; AID1559793
Melanocyte-stimulating hormone receptorHomo sapiens (human)IC50 (µMol)0.00050.00010.03760.6150AID108614; AID108616
Melanocyte-stimulating hormone receptorHomo sapiens (human)Ki0.00080.00000.00650.0370AID108622; AID632880; AID677158
Melanocyte-stimulating hormone receptorMus musculus (house mouse)IC50 (µMol)0.00030.00030.12950.3880AID1296528; AID1559787
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)EC50 (µMol)0.00010.00011.46937.0000AID109615
Adenosine receptor A2aRattus norvegicus (Norway rat)EC50 (µMol)0.00020.00000.11560.7200AID246687
Melanocortin receptor 3Rattus norvegicus (Norway rat)EC50 (µMol)0.00010.00010.00010.0001AID108945
Melanocortin receptor 4Homo sapiens (human)EC50 (µMol)0.00150.00000.09112.6000AID108957; AID108965; AID108967; AID108968; AID108969; AID108970; AID109107; AID109462; AID1476414; AID1476420; AID1479778; AID246687; AID259544; AID259545; AID259546; AID259547; AID259548; AID259549; AID259550; AID259551; AID259552; AID259553; AID677162; AID82381
Melanocortin receptor 5Homo sapiens (human)EC50 (µMol)0.00070.00020.16154.4000AID109296; AID109298; AID109299; AID109305; AID1476417; AID1479779; AID246688
Melanocortin receptor 3Mus musculus (house mouse)EC50 (µMol)0.00290.00010.28575.4000AID108937; AID108939; AID109614; AID109615; AID109617; AID1151525; AID1169943; AID1296535; AID1428575; AID1458955; AID1479773; AID1483074; AID1547511; AID1559777; AID1638718; AID1685034; AID1725372; AID1771948; AID1776305; AID221832; AID240040; AID240052; AID282351; AID321769; AID391356; AID447386; AID587930; AID729276
Melanocortin receptor 3Mus musculus (house mouse)Kd812,831.00000.00030.06730.1995AID1356510
Melanocortin receptor 5Mus musculus (house mouse)EC50 (µMol)0.00620.00000.03211.4900AID107044; AID107045; AID107046; AID109444; AID109446; AID109447; AID1151527; AID1296537; AID1356506; AID1428577; AID1458957; AID1479775; AID1483084; AID1547516; AID1559783; AID1638724; AID1685033; AID1725377; AID1771950; AID1776311; AID221835; AID240042; AID240054; AID282355; AID321771; AID391365; AID447388; AID587928; AID729274
Melanocortin receptor 3Homo sapiens (human)EC50 (µMol)0.00180.00010.01270.2480AID108777; AID108778; AID108779; AID108780; AID108781; AID108786; AID1476411; AID1479777; AID246686; AID82380
Melanocortin receptor 4Mus musculus (house mouse)EC50 (µMol)0.00460.00000.12472.4700AID107033; AID107034; AID107035; AID109275; AID109277; AID109279; AID1151526; AID1169944; AID1296536; AID1428576; AID1458956; AID1479774; AID1483077; AID1547514; AID1559780; AID1638719; AID1685035; AID1725375; AID1776308; AID221834; AID240041; AID240053; AID282353; AID321770; AID391362; AID447387; AID587929; AID729275
Melanocortin receptor 4Mus musculus (house mouse)Kd229,087.00000.00000.00180.0050AID1356511
Melanocyte-stimulating hormone receptorHomo sapiens (human)EC50 (µMol)0.00020.00000.00800.2280AID108481; AID108604; AID108605; AID108607; AID108611; AID109453; AID1479776; AID71942; AID82379
Melanocyte-stimulating hormone receptorMus musculus (house mouse)EC50 (µMol)0.00040.00000.30047.6900AID108634; AID108636; AID108637; AID109599; AID109601; AID109602; AID1151524; AID1169942; AID1296534; AID1356503; AID1428574; AID1458954; AID1479772; AID1483081; AID1547509; AID1559775; AID1638723; AID1685031; AID1725370; AID1771945; AID1776302; AID221830; AID240039; AID240051; AID282350; AID321787; AID391354; AID447385; AID587926; AID729277
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (89)

Processvia Protein(s)Taxonomy
adenosine catabolic processAdenosine deaminaseHomo sapiens (human)
inosine biosynthetic processAdenosine deaminaseHomo sapiens (human)
allantoin metabolic processAdenosine deaminaseHomo sapiens (human)
response to hypoxiaAdenosine deaminaseHomo sapiens (human)
trophectodermal cell differentiationAdenosine deaminaseHomo sapiens (human)
liver developmentAdenosine deaminaseHomo sapiens (human)
placenta developmentAdenosine deaminaseHomo sapiens (human)
germinal center B cell differentiationAdenosine deaminaseHomo sapiens (human)
germinal center formationAdenosine deaminaseHomo sapiens (human)
positive regulation of germinal center formationAdenosine deaminaseHomo sapiens (human)
negative regulation of leukocyte migrationAdenosine deaminaseHomo sapiens (human)
mature B cell apoptotic processAdenosine deaminaseHomo sapiens (human)
negative regulation of mature B cell apoptotic processAdenosine deaminaseHomo sapiens (human)
adenosine catabolic processAdenosine deaminaseHomo sapiens (human)
deoxyadenosine catabolic processAdenosine deaminaseHomo sapiens (human)
AMP catabolic processAdenosine deaminaseHomo sapiens (human)
xenobiotic metabolic processAdenosine deaminaseHomo sapiens (human)
smooth muscle contractionAdenosine deaminaseHomo sapiens (human)
cell adhesionAdenosine deaminaseHomo sapiens (human)
response to inorganic substanceAdenosine deaminaseHomo sapiens (human)
positive regulation of heart rateAdenosine deaminaseHomo sapiens (human)
response to purine-containing compoundAdenosine deaminaseHomo sapiens (human)
calcium-mediated signalingAdenosine deaminaseHomo sapiens (human)
positive regulation of B cell proliferationAdenosine deaminaseHomo sapiens (human)
purine nucleotide salvageAdenosine deaminaseHomo sapiens (human)
GMP salvageAdenosine deaminaseHomo sapiens (human)
T cell differentiation in thymusAdenosine deaminaseHomo sapiens (human)
positive regulation of T cell differentiation in thymusAdenosine deaminaseHomo sapiens (human)
regulation of cell-cell adhesion mediated by integrinAdenosine deaminaseHomo sapiens (human)
B cell proliferationAdenosine deaminaseHomo sapiens (human)
T cell activationAdenosine deaminaseHomo sapiens (human)
penile erectionAdenosine deaminaseHomo sapiens (human)
purine-containing compound salvageAdenosine deaminaseHomo sapiens (human)
amide catabolic processAdenosine deaminaseHomo sapiens (human)
AMP salvageAdenosine deaminaseHomo sapiens (human)
positive regulation of smooth muscle contractionAdenosine deaminaseHomo sapiens (human)
dAMP catabolic processAdenosine deaminaseHomo sapiens (human)
dATP catabolic processAdenosine deaminaseHomo sapiens (human)
adenosine metabolic processAdenosine deaminaseHomo sapiens (human)
inosine biosynthetic processAdenosine deaminaseHomo sapiens (human)
xanthine biosynthetic processAdenosine deaminaseHomo sapiens (human)
alpha-beta T cell differentiationAdenosine deaminaseHomo sapiens (human)
positive regulation of alpha-beta T cell differentiationAdenosine deaminaseHomo sapiens (human)
lung alveolus developmentAdenosine deaminaseHomo sapiens (human)
Peyer's patch developmentAdenosine deaminaseHomo sapiens (human)
embryonic digestive tract developmentAdenosine deaminaseHomo sapiens (human)
negative regulation of inflammatory responseAdenosine deaminaseHomo sapiens (human)
positive regulation of calcium-mediated signalingAdenosine deaminaseHomo sapiens (human)
T cell receptor signaling pathwayAdenosine deaminaseHomo sapiens (human)
positive regulation of T cell receptor signaling pathwayAdenosine deaminaseHomo sapiens (human)
leukocyte migrationAdenosine deaminaseHomo sapiens (human)
negative regulation of adenosine receptor signaling pathwayAdenosine deaminaseHomo sapiens (human)
negative regulation of penile erectionAdenosine deaminaseHomo sapiens (human)
thymocyte apoptotic processAdenosine deaminaseHomo sapiens (human)
negative regulation of thymocyte apoptotic processAdenosine deaminaseHomo sapiens (human)
mucus secretionAdenosine deaminaseHomo sapiens (human)
negative regulation of mucus secretionAdenosine deaminaseHomo sapiens (human)
hypoxanthine salvageAdenosine deaminaseHomo sapiens (human)
diet induced thermogenesisMelanocortin receptor 4Homo sapiens (human)
energy reserve metabolic processMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
feeding behaviorMelanocortin receptor 4Homo sapiens (human)
insulin secretionMelanocortin receptor 4Homo sapiens (human)
response to insulinMelanocortin receptor 4Homo sapiens (human)
positive regulation of bone resorptionMelanocortin receptor 4Homo sapiens (human)
regulation of eating behaviorMelanocortin receptor 4Homo sapiens (human)
response to melanocyte-stimulating hormoneMelanocortin receptor 4Homo sapiens (human)
negative regulation of feeding behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of grooming behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 5Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 5Homo sapiens (human)
regulation of heart rateMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
regulation of blood pressureMelanocortin receptor 3Homo sapiens (human)
circadian regulation of gene expressionMelanocortin receptor 3Homo sapiens (human)
homoiothermyMelanocortin receptor 3Homo sapiens (human)
locomotor rhythmMelanocortin receptor 3Homo sapiens (human)
sodium ion homeostasisMelanocortin receptor 3Homo sapiens (human)
regulation of feeding behaviorMelanocortin receptor 3Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocyte-stimulating hormone receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV protectionMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase A signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
sensory perception of painMelanocyte-stimulating hormone receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionMelanocyte-stimulating hormone receptorHomo sapiens (human)
intracellular signal transductionMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanin biosynthetic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
pigmentationMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV-damage excision repairMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase C signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of feeding behaviorMelanocyte-stimulating hormone receptorHomo sapiens (human)
regulation of metabolic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
adenosine deaminase activityAdenosine deaminaseHomo sapiens (human)
protein bindingAdenosine deaminaseHomo sapiens (human)
zinc ion bindingAdenosine deaminaseHomo sapiens (human)
deaminase activityAdenosine deaminaseHomo sapiens (human)
2'-deoxyadenosine deaminase activityAdenosine deaminaseHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2aRattus norvegicus (Norway rat)
melanocortin receptor activityMelanocortin receptor 4Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 4Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 4Homo sapiens (human)
ubiquitin protein ligase bindingMelanocortin receptor 4Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 5Homo sapiens (human)
hormone bindingMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 3Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 3Homo sapiens (human)
protein bindingMelanocortin receptor 3Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 3Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 3Homo sapiens (human)
melanocortin receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
protein bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
G protein-coupled peptide receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
ubiquitin protein ligase bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
hormone bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
lysosomeAdenosine deaminaseHomo sapiens (human)
cytosolAdenosine deaminaseHomo sapiens (human)
plasma membraneAdenosine deaminaseHomo sapiens (human)
external side of plasma membraneAdenosine deaminaseHomo sapiens (human)
cell surfaceAdenosine deaminaseHomo sapiens (human)
membraneAdenosine deaminaseHomo sapiens (human)
cytoplasmic vesicle lumenAdenosine deaminaseHomo sapiens (human)
anchoring junctionAdenosine deaminaseHomo sapiens (human)
cytosolAdenosine deaminaseHomo sapiens (human)
external side of plasma membraneAdenosine deaminaseHomo sapiens (human)
Golgi membraneAdenosine receptor A2aRattus norvegicus (Norway rat)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
membraneMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
cytoplasmMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
cytoplasmMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
cytoplasmMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (256)

Assay IDTitleYearJournalArticle
AID1559787Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1296529Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID729274Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano
AID108614Displacement of [125I]NDP-MSH from Melanocortin 1 receptor at 10 uM1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID321769Agonist activity at mouse MC3R expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID1547514Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID109601In vitro activation of mouse recombinant Melanocortin-1 receptor.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID108616Inhibitory concentration against human Melanocortin 1 receptor (hMC1R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1479773Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID109299Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID109305effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID108945Maximal agonist response at rat melanocortin 3 receptor (MC3R)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
AID1356511Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
AID1458955Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t
AID587926Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
AID252625Maximal effect on human melanocortin 5 receptor expressing HEK 293 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1559793Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1479776Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID447387Agonistic activity against mouse MC4R2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Semi-rigid tripeptide agonists of melanocortin receptors.
AID1725377Agonist activity at mouse MC5R by alphascreen cAMP assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Peptoid NPhe
AID246688Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108773Percent activation of human melanocortin receptor Melanocortin 3 receptor was determined at 10 uM2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID259549Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID1559799Displacement of [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1776305Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
AID259535Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108607Evaluated for agonist activity at cloned mammalian human MSH1 receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID109277Effective concentration against mouse melanocortin MC4 receptor2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID109111Binding affinity for Human Melanocortin 4 receptor expressed in L-cells2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID242174Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID109285Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-hAGRP(82-132); ND = not determined2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID82379In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
AID71945Relative potency compared to alpha MSH in a frog skin bioassay.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID1776302Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
AID109296Effective concentration of peptide at 50% maximal cAMP generation2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID108965Effective concentration of peptide at 50% maximal cAMP generation2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID109599Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID1725375Agonist activity at mouse MC4R by alphascreen cAMP assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Peptoid NPhe
AID259540Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109279Effective concentration for maximum agonist response towards mouse melanocortin 4 receptor2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
AID1476413Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID108636Effective concentration against mouse Melanocortin 1 receptor2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID391362Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
AID1559796Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1559777Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID107046Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID109447Maximum agonist response for mouse melanocortin 5 receptor (MC5R)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
AID82380In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
AID1725370Agonist activity at mouse MC1R by alphascreen cAMP assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Peptoid NPhe
AID71942Decrease in frog skin reflectivity (metabotropic activity).1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID33850Inhibition of human adenosine deaminase (ADA)2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Structure-based design, synthesis, and structure-activity relationship studies of novel non-nucleoside adenosine deaminase inhibitors.
AID259551Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID240051In vitro agonist potency for Mouse Melanocortin 1 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID259547Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109283Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID1428575Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
A Macrocyclic Agouti-Related Protein/[Nle
AID102011Decrease in lizard skin reflectivity (metabotropic activity).1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID1458956Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t
AID109446Effective concentration against mouse Melanocortin 5 receptor2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID108798Binding affinity towards human Melanocortin 3 receptor (hMC3R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
AID1559790Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1559780Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1356510Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as reduction in NDP-MSH-induced response incubated for 2 hrs by AlphaScreen cAMP assay based Schild analysis
AID252624Maximal effect on human melanocortin 4 receptor expressing HEK 293 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1296535Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID221830Functional activity at the mouse melanocortin 1 receptor2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID321787Agonist activity at mouse MC1R expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID1479772Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID108939Effective concentration against mouse Melanocortin 3 receptor2004Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9
Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID107034In vitro activation of mouse recombinant Melanocortin-4 receptor.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID1151527Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID259546Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID1356509Agonist activity at mouse MC4R expressed in HEK293 cells at 100 uM incubated for 2 hrs by AlphaScreen cAMP assay relative to untreated control
AID346427Displacement of radiolabeled NDPalpha-MSH from human MC4 receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID391354Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
AID259542Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109127Inhibitory activity against human Melanocortin 4 receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID1476417Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID282351Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID107033Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID240566Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 42005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108968Effective concentration required for the biological activity against human Melanocortin 4 receptor2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID1479774Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID259543Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108795Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID1476419Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID242173Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1483077Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID109614Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID1685034Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
AID677159Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID632881Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
AID108952Percent activation of human melanocortin receptor human Melanocortin 4 receptor was determined at 10 uM2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID109453Agonist activity against human melanocortin receptor hMC1R2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.
AID108622Binding affinity towards human Melanocortin 1 receptor (hMC1R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
AID246686Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1296527Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID447386Agonistic activity against mouse MC3R2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Semi-rigid tripeptide agonists of melanocortin receptors.
AID240039Effective concentration for mouse Melanocortin-1 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID108957Agonist potency towards human Melanocortin 4 receptor2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.
AID246687Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID259545Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108777Effective concentration of peptide at 50% maximal cAMP generation2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID1483081Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID109119Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID108937Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Urea small molecule agonists on mouse melanocortin receptors.
AID1483084Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID677161Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1483091Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID1151525Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID109107effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID677158Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1428576Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
A Macrocyclic Agouti-Related Protein/[Nle
AID108794Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID632884Selectivity ratio of Ki for human MC5 receptor expressed in human HEK293 cells to Ki for human MC1 receptor expressed in human HCT116 cells2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
AID1356503Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
AID677162Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID1169942Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1476411Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1771945Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.
AID751880Binding affinity to human MC4 receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID1151524Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID391356Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
AID259541Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID1476414Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID259534Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID240052In vitro agonist potency for Mouse Melanocortin 3 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID109602Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID109429Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID259544Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID259548Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108637Maximal agonist response of mouse melanocortin 1 receptor (MC1R)2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
AID108604Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID252623Maximal effect on human melanocortin 3 receptor expressing HEK 293 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID321771Agonist activity at mouse MC5R expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID108775Maximum accumulation of cAMP level against Melanocortin 3 receptor at 10 uM2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID1479778Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID240053In vitro agonist potency for Mouse Melanocortin 4 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID109425Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID259536Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109306Binding affinity for Human Melanocortin 5 receptor expressed in L-cells2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID107045In vitro activation of mouse recombinant Melanocortin-5 receptor.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID321768Displacement of [125I]NDP-alpha-MSH from MC4R2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID259537Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID282353Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID1356506Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay
AID1638719Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.
AID1483074Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID109462Agonist activity against human melanocortin receptor hMC4R2003Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.
AID1638723Full agonist activity at mouse MC1R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.
AID1479777Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID104102Effective concentration was measured against frog skin MCR cells at 10 e-4 10 e-12 M Concentration.1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID240040Effective concentration for mouse Melanocortin-3 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID1476421Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID729277Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano
AID732393Cytotoxicity against human HEK293 cells assessed as cell viability at 100 uM to 1 uM upto 48 hrs
AID108786effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID259553Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108481Agonist potency for human Melanocortin 1 receptor2002Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17
Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.
AID1685031Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
AID259552Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109617Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID102012In vitro potency of compound to stimulate melanosome dispersion in lizard skin relative to alpha-MSH1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID108781Evaluated for agonist activity at cloned Melanocortin 3 receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID221832Functional activity at the mouse melanocortin 3 receptor2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID1458954Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t
AID1685033Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
AID752240Binding affinity to human MC4 receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID109298Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID71943In vitro potency of compound to stimulate melanosome dispersion in frog (Rana pipiens) skin relative to alpha-MSH1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID108792Inhibition of human Melanocortin 3 receptor2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID108605Effective concentration required for the biological activity against human Melanocortin 1 receptor2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID109291Maximum accumulation of cAMP by Melanocortin 5 receptor at 10 uM2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID282350Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID109444Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Urea small molecule agonists on mouse melanocortin receptors.
AID1336329Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID282355Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID1296534Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID1771950Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.
AID108969Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID1483073Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting2017Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
AID102013Relative potency compared to alpha MSH in a lizard skin bioassay.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID677160Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID108956Maximum accumulation of cAMP level by Melanocortin 4 receptor at 10 uM2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID1285634Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID1479775Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID587930Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
AID221834Functional activity at the mouse melanocortin 4 receptor2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID1771948Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist.
AID240054In vitro agonist potency for Mouse Melanocortin 5 receptor2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID587928Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
AID108787Binding affinity for Human Melanocortin 3 receptor expressed in L-cells2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID447388Agonistic activity against mouse MC5R2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Semi-rigid tripeptide agonists of melanocortin receptors.
AID1776311Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
AID259538Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID107044Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID108611effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor1997Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R.
AID1685035Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
AID108778Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1169944Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID109131Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID321770Agonist activity at mouse MC4R expressed in HEK293 cells2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID240041Effective concentration for mouse Melanocortin-4 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID1547509Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID1705453Photo-protective activity in EPP patient assessed as time spent in direct sunlight without pain measured after 6 months (Rvb = 41 hrs)2020European journal of medicinal chemistry, Nov-01, Volume: 205New drug approvals for 2019: Synthesis and clinical applications.
AID109289Percent activation of human melanocortin receptor Melanocortin 5 receptor was determined at 10 uM2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID1725372Agonist activity at mouse MC3R by alphascreen cAMP assay2020ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
Peptoid NPhe
AID34307In vitro potency of compound to stimulate adenylate cyclase activity in melanoma cells relative to alpha-MSH1982Journal of medicinal chemistry, Sep, Volume: 25, Issue:9
Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID729276Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano
AID729275Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay2013Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
Structure-activity relationships of peptides incorporating a bioactive reverse-turn heterocycle at the melanocortin receptors: identification of a 5800-fold mouse melanocortin-3 receptor (mMC3R) selective antagonist/partial agonist versus the mouse melano
AID1547511Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID632883Selectivity ratio of Ki for human MC4 receptor expressed in human HEK293 cells to Ki for human MC1 receptor expressed in human HCT116 cells2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
AID1151529Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID108790Inhibitory activity against Melanocortin 3 receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID447385Agonistic activity against mouse MC1R2009Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
Semi-rigid tripeptide agonists of melanocortin receptors.
AID109275Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Urea small molecule agonists on mouse melanocortin receptors.
AID240042Effective concentration for mouse Melanocortin-5 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID632880Displacement of Eu-NDP-alphaMSH from human MC1 receptor expressed in human HCT116 cells after 1.5 hrs by time-resolved fluorescence analysis2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
AID1776308Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign.
AID1169943Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID391365Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity.
AID1638724Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.
AID1476416Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID259550Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID1296528Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID1476420Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID632882Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Development of melanoma-targeted polymer micelles by conjugation of a melanocortin 1 receptor (MC1R) specific ligand.
AID108780Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor2000Journal of medicinal chemistry, Dec-28, Volume: 43, Issue:26
D-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity.
AID108970Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptor1995Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID1638718Agonist activity at mouse MC3R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μM MC4R Partial Agonist.
AID108967Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1458957Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 10-12, Volume: 60, Issue:19
Structure-Activity Relationship Studies on a Macrocyclic Agouti-Related Protein (AGRP) Scaffold Reveal Agouti Signaling Protein (ASP) Residue Substitutions Maintain Melanocortin-4 Receptor Antagonist Potency and Result in Inverse Agonist Pharmacology at t
AID109428Inhibition of human melanocortin 5 receptor2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID1559775Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID1559783Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Incorporation of Agouti-Related Protein (AgRP) Human Single Nucleotide Polymorphisms (SNPs) in the AgRP-Derived Macrocyclic Scaffold c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-dPro] Decreases Melanocortin-4 Receptor Antagonist Potency and Results in the Discovery of M
AID109128Inhibition of human melanocortin 4 receptor2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID108779Effective concentration required for the biological activity against human Melanocortin 3 receptor2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID82381In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
AID252622Maximal effect on human melanocortin 1 receptor expressing HEK 293 cells2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1296537Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID1356508Agonist activity at mouse MC3R expressed in HEK293 cells at 100 uM incubated for 2 hrs by AlphaScreen cAMP assay relative to untreated control
AID1169945Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1547516Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay2020ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3
Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID1151528Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID259539Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells2006Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3
Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID587929Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay2011Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
Incorporation of a bioactive reverse-turn heterocycle into a peptide template using solid-phase synthesis to probe melanocortin receptor selectivity and ligand conformations by 2D 1H NMR.
AID108634Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells2003Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
Urea small molecule agonists on mouse melanocortin receptors.
AID1151526Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID1296536Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay2016Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID1428577Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
A Macrocyclic Agouti-Related Protein/[Nle
AID109615In vitro activation of mouse recombinant Melanocortin-3 receptor.2002Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID107035Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID221835Functional activity at the mouse melanocortin 5 receptor2001Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13
Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID1479779Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Human β-Defensin 1 and β-Defensin 3 (Mouse Ortholog mBD14) Function as Full Endogenous Agonists at Select Melanocortin Receptors.
AID1428574Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay2017Journal of medicinal chemistry, 01-26, Volume: 60, Issue:2
A Macrocyclic Agouti-Related Protein/[Nle
AID109137Binding affinity towards human melanocortin 4 receptor (hMC4R)2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (265)

TimeframeStudies, This Drug (%)All Drugs %
pre-199017 (6.42)18.7374
1990's63 (23.77)18.2507
2000's103 (38.87)29.6817
2010's70 (26.42)24.3611
2020's12 (4.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 9.31

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index9.31 (24.57)
Research Supply Index5.65 (2.92)
Research Growth Index4.96 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (9.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (2.55%)5.53%
Reviews4 (1.45%)6.00%
Case Studies2 (0.73%)4.05%
Observational1 (0.36%)0.25%
Other261 (94.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]